消化道酶类药物剂型研究—双糖酶肠溶微囊

人体肠道各种双糖酶均可因先天性或继发性缺乏而引起相应的双糖消化吸收障碍。其中乳糖酶缺乏在东方人种内普遍存在。所引起的不良影响,对处于哺乳期的婴幼儿尤为严重。用外源性的双糖酶口服以辅助双糖消化吸收是一个较好的治疗方法。但是,由于微生物来源的双糖酶在消化道易被胃酸和胃肠道蛋白酶破坏,国外在临床试验中曾采取高剂量酶制剂口服的方法,以保证有足够的双糖酶残留量进入小肠发挥作用。此法成本高且疗效不稳定。本文报道双糖酶肠溶微囊的研制。体外实验证实,本制剂能使双糖酶在人体小肠内释放而避免被胃液破坏。有希望用于双糖吸收障碍症的临床治疗。

An approach to the preparation of digestive enzyme-drug for oral administration: enteric-soluble disaccharidase microcapsules]

For the purpose of replacement therapy in cases of disaccharide intolerances, yeast disaccharidases were prepared as enteric-soluble microcapsules to prevent their inactivation by gastric juice and alimentary proteases. The enteric-soluble microcapsules have a mean diameter of 0.544 +/- 0.058 mm. Following encapsulation, activity recoveries for invertase and lactase were 84.4 +/- 10.6% and 70.1 +/- 5.5%, respectively. Over 55% of the remaining microcapsulated disaccharidase activity was retained in artificial gastric juice during 2 h of coincubation. Over 90% of the enzyme activity was released from the microcapsules within 1 h in artificial intestinal juice.